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奥拉西坦

奥拉西坦用途

Oxiracetam 是 γ-氨基丁酸 (GABA) 的环状衍生物,其已被普遍用作治疗认知障碍的益智药物。

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奥拉西坦名称

[ CAS 号 ]:
62613-82-5

[ 中文名 ]:
奥拉西坦

[ 英文名 ]:
Oxiracetam

[中文别名 ]:

[英文别名 ]:

4-Hydroxy-2-oxopyrrolidine-N-acetamide
2-(4-Hydroxypyrrolidin-2-on-1-yl)acetamide
MFCD00242951
oxiracetam
1-Pyrrolidineacetamide, 4-hydroxy-2-oxo-
2-(4-hydroxy-2-oxopyrrolidin-1-yl)acetamide
2-(4-Hydroxy-2-oxo-1-pyrrolidinyl)acetamide
UNII:P7U817352G

奥拉西坦生物活性

[ 描述 ]:

Oxiracetam 是 γ-氨基丁酸 (GABA) 的环状衍生物,其已被普遍用作治疗认知障碍的益智药物。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

研究领域 >> 神经疾病

[ 靶点 ]

GABA receptor[1]

[参考文献]

[1]. Li W, et al. (S)-Oxiracetam is the Active Ingredient in Oxiracetam that Alleviates the Cognitive Impairment Induced by Chronic Cerebral Hypoperfusion in Rats. Sci Rep. 2017 Aug 30;7(1):10052.

[相关活性小分子]

奥拉西坦物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
494.6±40.0 °C at 760 mmHg

[ 熔点 ]:
165-168ºC

[ 分子式 ]:
C₆H₁₀N₂O₃

[ 分子量 ]:
158.155

[ 闪点 ]:
252.9±27.3 °C

[ 精确质量 ]:
158.069138

[ PSA ]:
83.63000

[ LogP ]:
-2.48

[ 外观性状 ]:
白色到黄色粉末或晶体

[ 蒸汽压 ]:
0.0±2.9 mmHg at 25°C

[ 折射率 ]:
1.570

[ 储存条件 ]:
2-8°C

奥拉西坦MSDS

详细MSDS(安全技术说明书)

奥拉西坦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UX9656638

CHEMICAL NAME :: 1-Pyrrolidineacetamide, 4-hydroxy-2-oxo-

CAS REGISTRY NUMBER :: 62613-82-5

BEILSTEIN REFERENCE NO. :: 1529719

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C6-H10-N2-O3

MOLECULAR WEIGHT :: 158.18

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,405,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 182 gm/kg/52W-C

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3519,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 22 gm/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - delayed effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 19,3545,1991

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奥拉西坦安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319

[ 警示性声明 ]:
P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UX9656638

[ 海关编码 ]:
2933790090

奥拉西坦上下游产品

奥拉西坦上游产品

奥拉西坦下游产品

奥拉西坦制备

生产方法一：4-氨基-3-羟基丁酸和二(三甲基硅烷基)胺反应，对羟基进行保护，然后内酰胺化生成内酰胺，以2-溴乙酸乙酯对氨基进行烷基化，生成2-氧代-4-三甲硅氧基-1-吡咯烷乙酸乙酯，水解脱去羟基上的保护基，再氨解得到奥拉西坦。
生产方法二：648g亚胺二乙酸乙酯溶于3600ml无水二氯甲烷和572ml三乙胺中，在0℃和搅拌下，滴加619g 2-乙酯基乙酰氯溶于1100ml二氯甲烷中的溶液。在滴加过程中，注意反应温度不要超过10～15℃。加毕，在室温下搅拌2h后，放置过夜。然后水洗，干燥，减压浓缩。得到的油状的N-(2-乙酯基乙酰基)亚胺二乙酸乙酯溶于无水苯中，然后在室温下，把该苯溶液加到75.6g钠溶于2700ml无水乙醇的溶液。回流6h，冷却至室温。用水不断地萃取反应液，萃取液合并，用盐酸酸化至Ph值为1。过滤析出的沉淀，重结晶得2-(3-乙酯基-4羟基-△3-吡咯烷-2-酮-1-基)乙酸乙酯，熔点175～179℃。
将20g 2-(3-乙酯基-4-羟基-△3-吡咯烷-2-酮-1-基)乙酸乙酯加入200ml热乙腈和1.8ml水中。回流20min后，用冰浴冷却，减压浓缩得2-(吡咯烷-2，4-二酮-1-基)乙酸乙酯，熔点87～91℃。
将22.25g 2-(吡咯烷-2，4-二酮-1-基)乙酸乙酯溶于445ml无水二甲氧基乙烷中，冷至0℃，加入1.52g硼氢化钠，在冰浴上放置：10min后，再在室温下放置30min。用20%盐酸酸化，过滤，滤液减压浓缩后，溶入二氯甲烷，用无水硫酸镁干燥。过滤，减压浓缩，层析后得2-(4-羟基吡咯烷-2-酮-1-基)乙酸乙酯，熔点180℃(分解)。
8.9g 2-(4-羟基吡咯烷-2-酮-1-基)乙酸乙酯溶于300ml甲醇，在0℃时通入氨气，然后放置过夜。减压除去溶剂，剩余物溶入甲醇，用活性炭过滤。将滤液缓慢加到200ml异丙醚中，收集析出的沉淀，即为奥拉西坦，熔点16l～163℃。

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奥拉西坦海关

[ 海关编码 ]: 2933790090

[ 中文概述 ]:
2933790090 其他内酰胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:9.0% 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

奥拉西坦文献

Minaprine, but not oxiracetam, prevents desipramine-induced impairment of avoidance learning in mice.

Pol. J. Pharmacol. 47(1) , 69-73, (1995)

The tricyclic antidepressant desipramine impaired shuttle-box avoidance acquisition in mice of the CD-1 strain. The nootropic drug oxiracetam was unable to prevent the desipramine-induced learning imp...

Pre- and postprandial pyridostigmine and oxiracetam effects on growth hormone secretion in anorexia nervosa.

Psychoneuroendocrinology 21(7) , 621-9, (1996)

Previous studies have shown that food ingestion is not capable of inhibiting the GHRH-induced GH release in anorexia nervosa, at variance with what is observed in normal subjects. Moreover, a choliner...

Putative cognition enhancers reverse kynurenic acid antagonism at hippocampal NMDA receptors.

Eur. J. Pharmacol. 272(2-3) , 203-9, (1995)

Oxiracetam, aniracetam and D-cycloserine, three putative cognition enhancers, were examined in a functional assay for NMDA receptors. Rat hippocampal slices or synaptosomes were labeled with [3H]norad...

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奥拉西坦

奥拉西坦用途

奥拉西坦名称

奥拉西坦生物活性

奥拉西坦物理化学性质

奥拉西坦MSDS

详细MSDS(安全技术说明书)

奥拉西坦毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

奥拉西坦安全信息

奥拉西坦上下游产品

奥拉西坦上游产品

奥拉西坦下游产品

奥拉西坦制备

奥拉西坦海关

奥拉西坦文献

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